BONGARTZ, JEAN-PIERRE ANDRE MARC,邦加茨,VAN LOMMEN, GUY ROSALIA EUGEEN,凡洛门,凡洛門,COESEMANS, ERWIN,克思曼,BUYCK, CHRISTOPHE FRANCIS ROBERT NESTOR,拜克里
申请号:
TW097121017
公开号:
TWI436989B
申请日:
2008.06.06
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
The invention relates to a DGAT inhibitor of formulaincluding any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; -NRx-C(=O)-;-C(=O)-NRx-;-NRx-C(=O)-Z-;-NRx-C(=O)-Z-NRy-;-NRx-C(=O)-Z-NRy-C(=O)-;-NRx-C(=O)-Z-NRy-C(=O)-O-;-NRx-C(=O)-Z-O-;-NRx-C(=O)-Z-O-C(=O)-;-NRx-C(=O)-Z-C(=O)-;-NRx-C(=O)-Z-C(=O)-O-;-NRx-C(=O)-O-Z-C(=O)-;-NRx-C(=O)-O-Z-C(=O)-O-;-NRx-C(=O)-O-Z-O-C(=O)-;-NRx-C(=O)-Z-C(=O)-NRy-;-NRx-C(=O)-Z-NRy-C(=O)-NRy-;-C(=O)-Z-;-C(=O)-Z-O-;-C(=O)-NRx-Z-;-C(=O)-NRx-Z-O-;-C(=O)-NRx-Z-C(=O)-O-;-C(=O)-NRx-Z-O-C(=O)-;-C(=O)-NRx-O-Z-;-C(=O)-NRx-Z-NRy-;-C(=O)-NRx-Z-NRy-C(=O)-;-C(=O)-NRx-Z-NRy-C(=O)-O-;R1represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents -NRx-C(=O)-Z-;-NRx-C(=O)-Z-NRy;-NRx-C(=O)-Z-C(=O)-NRy-;-C(=O)-Z-;-NRx-C(=O)-Z-NRy-C(=O)-NRy-;-C(=O)-NRx-Z-;-C(=O)-NRx-O-Z-; or -C(=O)-NRx-Z-NRy-; then R1may also represent hydrogen; R2and R3each independently represent hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; C1-6alkyloxy optionally substituted with C1-4alkyloxy; C1-6alkylthio; polyhaloC1-6alkyloxy; C1-6alkyloxycarbonyl; cyano; aminocarbonyl; mono-or di(C1-4alkyl)aminocarbonyl; C1-6alkylcarbonyl; nitro; amino; mono-or di(C1-4alkyl)amino; -S(=O)p-C1-4alkyl; R4represents hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; C1-6alkylthio; polyhalo-C1-6alkyloxy; C1-6alkyloxycarbonyl wherein C1-6alkyl may optionally be substituted; cyano; C1-6alkylcarbonyl; nitro; amino; mono-or di(C1-4alkyl)amino; C1-4alkylcarbonylamino; -S(=O)p-C1-4alkyl; R6R5N-C(=O)-; R6R5N-C1-6